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[PMID]:29274490
[Au] Autor:Ghawanmeh AA; Chong KF; Sarkar SM; Bakar MA; Othaman R; Khalid RM
[Ad] Endereço:Faculty of Industrial Sciences & Technology, University Malaysia Pahang, Gambang, 26300 Kuantan, Pahang, Malaysia. Electronic address: gh.just4chem@hotmail.com.
[Ti] Título:Colchicine prodrugs and codrugs: Chemistry and bioactivities.
[So] Source:Eur J Med Chem;144:229-242, 2018 Jan 20.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:Antimitotic colchicine possesses low therapeutic index due to high toxicity effects in non-target cell. However, diverse colchicine analogs have been derivatized as intentions for toxicity reduction and structure-activity relationship (SAR) studying. Hybrid system of colchicine structure with nontoxic biofunctional compounds modified further affords a new entity in chemical structure with enhanced activity and selectivity. Moreover, nanocarrier formulation strategies have been used for colchicine delivery. This review paper focuses on colchicine nanoformulation, chemical synthesis of colchicine prodrugs and codrugs with different linkers, highlights linker chemical nature and biological activity of synthesized compounds. Additionally, classification of colchicine prodrugs based on type of conjugates is discussed, as biopolymers prodrugs, fluorescent prodrug, metal complexes prodrug, metal-labile prodrug and bioconjugate prodrug. Finally, we briefly summarized the biological importance of colchicine nanoformulation, colchicine prodrugs and codrugs.
[Mh] Termos MeSH primário: Colchicina/análogos & derivados
Colchicina/farmacologia
Pró-Fármacos/química
Pró-Fármacos/farmacologia
Moduladores de Tubulina/química
Moduladores de Tubulina/farmacologia
[Mh] Termos MeSH secundário: Animais
Desenho de Drogas
Seres Humanos
Mitose/efeitos dos fármacos
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Prodrugs); 0 (Tubulin Modulators); SML2Y3J35T (Colchicine)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180309
[Lr] Data última revisão:
180309
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171224
[St] Status:MEDLINE


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[PMID]:29268130
[Au] Autor:Lin HY; Han HW; Sun WX; Yang YS; Tang CY; Lu GH; Qi JL; Wang XM; Yang YH
[Ad] Endereço:State Key Laboratory of Pharmaceutical Biotechnology, NJU-NJFU Institute of Plant Molecular Biology, School of Life Sciences, Nanjing University, Nanjing, 210023, China; Co-Innovation Center for Sustainable Forestry in Southern China, Nanjing Forestry University, Nanjing, 210037, China.
[Ti] Título:Design and characterization of α-lipoic acyl shikonin ester twin drugs as tubulin and PDK1 dual inhibitors.
[So] Source:Eur J Med Chem;144:137-150, 2018 Jan 20.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:Shikonin exhibits powerful anticancer activities for various cancer cells, but its poor solubility and strong toxicity hinder its development as clinical anticancer agent. We previously confirmed that shikonin and its derivatives can disturb mitosis through targeting tubulin. In this study, α-lipoic acid, the naturally-occurring co-factor of pyruvate dehydrogenase (PDH), was introduced into shikonin to design the twin drugs against both mitosis (tubulin) and glycolysis (PDK). 18 kinds of α-lipoic acid shikonin ester derivatives were achieved through three rounds of screening process performed by computer assistant drug design method, being designated as the outstanding compounds. Among them, 1c displayed the most potent cytotoxicity towards cervical cancer cells (HeLa) with an IC value of 3.14 ± 0.58 µM and inhibited xenotransplanted tumor growth in a dose-dependent manner. Further pharmacologic study demonstrated that 1c can cause cell cycle arrest in G2/M phase as tubulin polymerization inhibitor. Moreover, it also showed good PDK1 inhibitory activity, promoting PDH activity and forced HeLa cells to process more aerobic metabolism to undergo cell apoptosis. We reported here the first dual inhibitors of tubulin and PDK1 based on shikonin. It may form a basis for shikonin optimization through twin drug design framework for the discovery of new and potent shikonin derivatives in the study of targeted cancer therapy.
[Mh] Termos MeSH primário: Antineoplásicos/química
Antineoplásicos/farmacologia
Naftoquinonas/química
Naftoquinonas/farmacologia
Proteínas Serina-Treonina Quinases/antagonistas & inibidores
Moduladores de Tubulina/química
Moduladores de Tubulina/farmacologia
[Mh] Termos MeSH secundário: Apoptose/efeitos dos fármacos
Pontos de Checagem do Ciclo Celular/efeitos dos fármacos
Desenho de Drogas
Glicólise/efeitos dos fármacos
Células HeLa
Seres Humanos
Mitose/efeitos dos fármacos
Neoplasias/tratamento farmacológico
Neoplasias/metabolismo
Proteínas Serina-Treonina Quinases/metabolismo
Tubulina (Proteína)/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Naphthoquinones); 0 (Tubulin); 0 (Tubulin Modulators); 3IK6592UBW (shikonin); EC 2.7.11.1 (Protein-Serine-Threonine Kinases); EC 2.7.11.2 (pyruvate dehydrogenase (acetyl-transferring) kinase)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180309
[Lr] Data última revisão:
180309
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171222
[St] Status:MEDLINE


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[PMID]:29268127
[Au] Autor:Khan I; Garikapati KR; Shaik AB; Makani VKK; Rahim A; Shareef MA; Reddy VG; Pal-Bhadra M; Kamal A; Kumar CG
[Ad] Endereço:Medicinal Chemistry and Biotechnology Division, CSIR-Indian Institute of Chemical Technology (IICT), Hyderabad 500007, India; Academy of Scientific and Innovative Research, New Delhi 110 025, India.
[Ti] Título:Design, synthesis and biological evaluation of 1, 4-dihydro indeno[1,2-c] pyrazole linked oxindole analogues as potential anticancer agents targeting tubulin and inducing p53 dependent apoptosis.
[So] Source:Eur J Med Chem;144:104-115, 2018 Jan 20.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:A series of 1, 4-dihydroindeno-[1,2-c] pyrazole linked oxindole conjugates have been synthesized by using Knoevenagel condensation method and further evaluated for their antiproliferative activity against HeLa, A549 and MDA-MB-231 human cancer cell lines along with HEK-293 (normal human embryonic kidney cells). Among the derivatives, compounds 12a, 12b, and 12d showed excellent cytotoxicity with IC values ranging between 1.33 to 4.33 µM. Furthermore, detailed biological assays showed that there was accumulation of mitotic cells in G2/M phase, disruption of microtubule network and increase in the G2/M checkpoint proteins (Cyclin B1 and CDK1). Moreover, compound 12d with IC value of 1.33 µM showed significant upregulation of tumor suppressor proteins like p53, p21 and pro-apoptotic Bax. The molecular docking analysis demonstrated that these congeners occupy the colchicine binding pocket of the tubulin.
[Mh] Termos MeSH primário: Antineoplásicos/química
Antineoplásicos/farmacologia
Apoptose/efeitos dos fármacos
Pirazóis/química
Pirazóis/farmacologia
Moduladores de Tubulina/química
Moduladores de Tubulina/farmacologia
[Mh] Termos MeSH secundário: Linhagem Celular Tumoral
Desenho de Drogas
Ensaios de Seleção de Medicamentos Antitumorais
Pontos de Checagem da Fase G2 do Ciclo Celular/efeitos dos fármacos
Células HEK293
Células HeLa
Seres Humanos
Indóis/química
Indóis/farmacologia
Simulação de Acoplamento Molecular
Neoplasias/tratamento farmacológico
Neoplasias/metabolismo
Tubulina (Proteína)/metabolismo
Proteína Supressora de Tumor p53/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Indoles); 0 (Pyrazoles); 0 (Tubulin); 0 (Tubulin Modulators); 0 (Tumor Suppressor Protein p53); 0S9338U62H (2-oxindole)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180309
[Lr] Data última revisão:
180309
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171222
[St] Status:MEDLINE


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[PMID]:29306206
[Au] Autor:Zhou P; Liang Y; Zhang H; Jiang H; Feng K; Xu P; Wang J; Wang X; Ding K; Luo C; Liu M; Wang Y
[Ad] Endereço:School of Pharmacy, Fudan University, Shanghai 201203, China; State Key Laboratory of Organometallic Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, Shanghai 200032, China.
[Ti] Título:Design, synthesis, biological evaluation and cocrystal structures with tubulin of chiral ß-lactam bridged combretastatin A-4 analogues as potent antitumor agents.
[So] Source:Eur J Med Chem;144:817-842, 2018 Jan 20.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:A diverse of chiral ß-lactam bridged analogues of combretastatin A-4 (CA-4), 3-substituted 1,4-diaryl-2-azetidinones, were asymmetrically synthesized and biologically evaluated, leading to identify a number of potent anti-proliferative compounds represented by 14b and 14c with IC values of 0.001-0.021 µM, against four human cancer cell lines (A2780, Hela, SKOV-3 and MDA-MB-231). Structure-activity relationship (SAR) studies on all stereoisomers of 14b and 14c revealed that the absolute configurations of the chiral centers at 3- and 4-position were critically important for the activity and generally a trans configuration between the "A" and "B" rings is optimal. In addition, 14b and 14c displayed less cytotoxicity on normal human oviduct epithelial cells than malignant cells indicating good selectivity in vitro. Further biochemical evaluation and cocrystal structures with tubulin demonstrated that both compounds disrupted tubulin polymerization through interacting at the colchicine-binding site, suppressed angiogenesis in vitro and in vivo, blocked cell cycle progression at mitotic phase and induced cellular apoptosis. The in vivo assays verified that both compounds inhibited xenograft tumor growth in nude mice with acceptable therapeutic window, showing promising potentials for further clinical development.
[Mh] Termos MeSH primário: Antineoplásicos/farmacologia
Desenho de Drogas
Estilbenos/farmacologia
Moduladores de Tubulina/farmacologia
Tubulina (Proteína)/química
beta-Lactamas/farmacologia
[Mh] Termos MeSH secundário: Animais
Antineoplásicos/síntese química
Antineoplásicos/química
Apoptose/efeitos dos fármacos
Ciclo Celular/efeitos dos fármacos
Proliferação Celular/efeitos dos fármacos
Cristalografia por Raios X
Relação Dose-Resposta a Droga
Ensaios de Seleção de Medicamentos Antitumorais
Feminino
Células HeLa
Seres Humanos
Camundongos
Camundongos Endogâmicos
Camundongos Nus
Modelos Moleculares
Estrutura Molecular
Neoplasias Experimentais/tratamento farmacológico
Neoplasias Experimentais/patologia
Polimerização/efeitos dos fármacos
Estilbenos/química
Relação Estrutura-Atividade
Tubulina (Proteína)/metabolismo
Moduladores de Tubulina/síntese química
Moduladores de Tubulina/química
beta-Lactamas/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Stilbenes); 0 (Tubulin); 0 (Tubulin Modulators); 0 (beta-Lactams); I5590ES2QZ (fosbretabulin)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180302
[Lr] Data última revisão:
180302
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180107
[St] Status:MEDLINE


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[PMID]:29291446
[Au] Autor:Stefanski T; Mikstacka R; Kurczab R; Dutkiewicz Z; Kucinska M; Murias M; Zielinska-Przyjemska M; Cichocki M; Teubert A; Kaczmarek M; Hogendorf A; Sobiak S
[Ad] Endereço:Department of Chemical Technology of Drugs, Poznan University of Medical Sciences, Grunwaldzka 6, 60-780 Poznan, Poland. Electronic address: tstefanski@ump.edu.pl.
[Ti] Título:Design, synthesis, and biological evaluation of novel combretastatin A-4 thio derivatives as microtubule targeting agents.
[So] Source:Eur J Med Chem;144:797-816, 2018 Jan 20.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:A series of novel combretastatin A-4 (CA-4) thio derivatives containing different molecular cores, namely α-phenylcinnamic acids (core 1), (Z)-stilbenes (core 2), 4,5-disubstituted oxazoles (core 3), and 4,5-disubstituted N-methylimidazoles (core 4), as cis-restricted analogues were designed and synthesized. They were selected with the use of a parallel virtual screening protocol including the generation of a virtual combinatorial library based on an elaborated synthesis protocol of CA-4 analogues. The selected compounds were evaluated for antiproliferative activity against a panel of six human cancer cell lines (A431, HeLa, MCF7, MDA-MB-231, A549 and SKOV) and two human non-cancer cell lines (HaCaT and CCD39Lu). Moreover, the effect of the test compounds on the inhibition of tubulin polymerization in vitro was estimated. In the series studied here, oxazole-bridged analogues exhibited the most potent antiproliferative activity. Compounds 23a, 23e, and 23i efficiently inhibited tubulin polymerization with IC values of 0.86, 1.05, and 0.85 µM, respectively. Thio derivative 23i, when compared to its oxygen analogue 23j, showed a 5-fold higher inhibitory impact on tubulin polymerization. Compounds 23e and 23i, which showed both best cytotoxic and antitubulin activity, were further studied in terms of their effect on cell cycle distribution and proapoptotic activity. Compound 23e induced a statistically significant block of the cell cycle at the G2/M phase in A431, HaCaT, HeLa, MCF-7, MDA-MB-231, and SKOV-3 cells to an extent comparable to that observed in CA-4. In HeLa and SKOV-3 cells incubated with 23i, a concentration-dependent block of the G2/M phase was observed. The proapoptotic effect of 23e and 23i in A431, HaCaT, MCF-7, MDA-MB-231, and SKOV-3 was demonstrated with ELISA assay and double staining with Annexin V-FITC/PI. The results indicated that compound 23e and 23i may serve as novel lead compounds in research on more effective anticancer agents.
[Mh] Termos MeSH primário: Antineoplásicos/farmacologia
Desenho de Drogas
Microtúbulos/efeitos dos fármacos
Estilbenos/farmacologia
Moduladores de Tubulina/farmacologia
[Mh] Termos MeSH secundário: Antineoplásicos/síntese química
Antineoplásicos/química
Ciclo Celular/efeitos dos fármacos
Linhagem Celular
Proliferação Celular/efeitos dos fármacos
Técnicas de Química Combinatória
Relação Dose-Resposta a Droga
Ensaios de Seleção de Medicamentos Antitumorais
Seres Humanos
Estrutura Molecular
Polimerização/efeitos dos fármacos
Estilbenos/síntese química
Estilbenos/química
Relação Estrutura-Atividade
Tubulina (Proteína)/metabolismo
Moduladores de Tubulina/síntese química
Moduladores de Tubulina/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Stilbenes); 0 (Tubulin); 0 (Tubulin Modulators); I5590ES2QZ (fosbretabulin)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180302
[Lr] Data última revisão:
180302
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180102
[St] Status:MEDLINE


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[PMID]:29395083
[Au] Autor:Yamagishi Y; Oya K; Matsuura A; Abe H
[Ad] Endereço:Department of Nanobiology, Graduate School of Advanced Integration Science, Chiba University, Chiba 263-8522, Japan. Electronic address: afha3649@chiba-u.jp.
[Ti] Título:Use of CK-548 and CK-869 as Arp2/3 complex inhibitors directly suppresses microtubule assembly both in vitro and in vivo.
[So] Source:Biochem Biophys Res Commun;496(3):834-839, 2018 02 12.
[Is] ISSN:1090-2104
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Two types of Arp2/3 complex inhibitors, CK-666/636 and CK-548/869, are commonly used to study Arp2/3 complex-dependent actin assembly both in vitro and in vivo. However, we found that CK-548 and CK-869 directly suppress microtubule (MT) assembly independent of the actin cytoskeleton. Treatment of cultured mammalian cells with 50 µM CK-869 dramatically decreased MT networks and, instead, accumulated tubulin at the cell periphery, as did nocodazole that inhibits MT assembly. An in vitro MT-sedimentation assay revealed that CK-548 and CK-869 significantly suppressed MT polymerization. In budding yeast, although CK-548 and CK-869 are reported to lack binding abilities in the yeast Arp3, CK-548 treatment decreased cytoplasmic MT at several tens of micromolar concentrations. In addition, we found that the effects of CK-548 and CK-869 on MT assembly varied according to species. We propose that CK-548 and CK-869 are not suitable for studying the cytoskeleton in living cells.
[Mh] Termos MeSH primário: Complexo 2-3 de Proteínas Relacionadas à Actina/antagonistas & inibidores
Complexo 2-3 de Proteínas Relacionadas à Actina/metabolismo
Microtúbulos/fisiologia
Compostos Organosselênicos/administração & dosagem
Compostos de Organossilício/administração & dosagem
Tiazóis/administração & dosagem
Tubulina (Proteína)/metabolismo
[Mh] Termos MeSH secundário: Animais
Relação Dose-Resposta a Droga
Drosophila melanogaster/metabolismo
Fibroblastos/efeitos dos fármacos
Fibroblastos/fisiologia
Gálio
Índio
Camundongos
Microtúbulos/efeitos dos fármacos
Células NIH 3T3
Ratos
Saccharomyces cerevisiae/metabolismo
Especificidade da Espécie
Moduladores de Tubulina
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Actin-Related Protein 2-3 Complex); 0 (CK-0993548); 0 (CK-869); 0 (In(0.3)Ga(0.7)N); 0 (Organoselenium Compounds); 0 (Organosilicon Compounds); 0 (Thiazoles); 0 (Tubulin); 0 (Tubulin Modulators); 045A6V3VFX (Indium); CH46OC8YV4 (Gallium)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180222
[Lr] Data última revisão:
180222
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180204
[St] Status:MEDLINE


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[PMID]:28467385
[Au] Autor:Field JJ; Northcote PT; Paterson I; Altmann KH; Díaz JF; Miller JH
[Ad] Endereço:Centre for Biodiscovery and Schools, Victoria University of Wellington, PO Box 600, Wellington 6140, New Zealand. jessica.field.nz@gmail.com.
[Ti] Título:Zampanolide, a Microtubule-Stabilizing Agent, Is Active in Resistant Cancer Cells and Inhibits Cell Migration.
[So] Source:Int J Mol Sci;18(5), 2017 May 03.
[Is] ISSN:1422-0067
[Cp] País de publicação:Switzerland
[La] Idioma:eng
[Ab] Resumo:Zampanolide, first discovered in a sponge extract in 1996 and later identified as a microtubule-stabilizing agent in 2009, is a covalent binding secondary metabolite with potent, low nanomolar activity in mammalian cells. Zampanolide was not susceptible to single amino acid mutations at the taxoid site of ß-tubulin in human ovarian cancer 1A9 cells, despite evidence that it selectively binds to the taxoid site. As expected, it did not synergize with other taxoid site microtubule-stabilizing agents (paclitaxel, ixabepilone, discodermolide), but surprisingly also did not synergize in 1A9 cells with laulimalide/peloruside binding site agents either. Efforts to generate a zampanolide-resistant cell line were unsuccessful. Using a standard wound scratch assay in cell culture, it was an effective inhibitor of migration of human umbilical vein endothelial cells (HUVEC) and fibroblast cells (D551). These properties of covalent binding, the ability to inhibit cell growth in paclitaxel and epothilone resistant cells, and the ability to inhibit cell migration suggest that it would be of interest to investigate zampanolide in preclinical animal models to determine if it is effective in vivo at preventing tumor growth and metastasis.
[Mh] Termos MeSH primário: Movimento Celular/efeitos dos fármacos
Proliferação Celular/efeitos dos fármacos
Resistência a Medicamentos Antineoplásicos/efeitos dos fármacos
Macrolídeos/farmacologia
Moduladores de Tubulina/farmacologia
[Mh] Termos MeSH secundário: Compostos Bicíclicos Heterocíclicos com Pontes/farmacologia
Linhagem Celular Tumoral
Feminino
Fibroblastos/efeitos dos fármacos
Células Endoteliais da Veia Umbilical Humana/efeitos dos fármacos
Seres Humanos
Lactonas/farmacologia
Microtúbulos/metabolismo
Taxoides/metabolismo
Tubulina (Proteína)/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Bridged Bicyclo Compounds, Heterocyclic); 0 (Lactones); 0 (Macrolides); 0 (Taxoids); 0 (Tubulin); 0 (Tubulin Modulators); 0 (laulimalide); 0 (peloruside A); 0 (zampanolide)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180221
[Lr] Data última revisão:
180221
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170504
[St] Status:MEDLINE


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[PMID]:29402238
[Au] Autor:Tanyildiz B; Tezcan ME; Kandemir B; Günaydin NT; Göktas E; Tangilntiz A; Arsan AK
[Ad] Endereço:Dr. Lutfi Kirdar Kartal Education and Research Hospital, Department of Ophthalmology, Semsi Denizer Caddesi, E-5, 34890, Kartal Istanbul, Turkey. buraktanyildiz@yahoo.com.
[Ti] Título:Effect of oral Colchicine on Peripapillary retinal nerve fiber layer thickness in patients with familial Mediterranean fever.
[So] Source:BMC Ophthalmol;18(1):27, 2018 Feb 05.
[Is] ISSN:1471-2415
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: The purpose of this study is to investigate whether oral colchicine has an effect on peripapillary retinal nerve fiber layer (pRNFL) thickness of familial Mediterranean fever (FMF) patients. METHODS: We conducted a cross sectional study by comparing pRNFL thickness of FMF patients on colchicine (treated group), newly diagnosed colchicine naïve FMF patients (untreated group) and healthy controls. The study included 66 FMF patients and 32 healthy control subjects. Treated FMF patients were grouped according to colchicine use, duration of use and dosage. pRNFL thickness of the patients and controls were measured by using optical coherence tomography and the measurements were compared. RESULTS: No statistically significant difference was found between the pRNFL thickness in untreated group, treated group and the healthy control group (all p > 0.05). No statistically significant difference was found between pRNFL thickness in the healthy control group and FMF patients grouped according to duration or dosage of colchicine use (all p > 0.05). CONCLUSIONS: According to our study, FMF and oral colchicine use had no statistically significant effect on pRNFL thickness.
[Mh] Termos MeSH primário: Colchicina/uso terapêutico
Febre Familiar do Mediterrâneo/tratamento farmacológico
Fibras Nervosas/efeitos dos fármacos
Células Ganglionares da Retina/efeitos dos fármacos
Moduladores de Tubulina/uso terapêutico
[Mh] Termos MeSH secundário: Administração Oral
Adulto
Estudos Transversais
Feminino
Seres Humanos
Pressão Intraocular
Masculino
Meia-Idade
Fibras Nervosas/patologia
Disco Óptico
Células Ganglionares da Retina/patologia
Tomografia de Coerência Óptica
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Tubulin Modulators); SML2Y3J35T (Colchicine)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180216
[Lr] Data última revisão:
180216
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180207
[St] Status:MEDLINE
[do] DOI:10.1186/s12886-018-0698-1


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[PMID]:29374936
[Au] Autor:Ni ZH; Huang WH; Liu Y; Chen ZJ; Li J; Yang JQ; He PC; Zhou YL; Chen JY; Luo JF
[Ad] Endereço:Department of Cardiology, Guangdong General Hospital, Guangdong Academy of Medical Science, Guangdong Provincial Key Laboratory of Coronary Heart Disease Prevention, Guangdong Cardiovascular Institute, Guangzhou 510080, China.
[Ti] Título:[Feasibility and safety of paclitaxel-eluting balloon for the treatment of de novo coronary lesions].
[So] Source:Zhonghua Xin Xue Guan Bing Za Zhi;46(1):39-43, 2018 Jan 24.
[Is] ISSN:0253-3758
[Cp] País de publicação:China
[La] Idioma:chi
[Ab] Resumo:To evaluate the safety and feasibility of treating de novo coronary lesions with paclitaxel-eluting balloon. This is a retrospective study, which enrolled 76 patients with 80 de novo coronary lesions treated with paclitaxel-eluting balloons(<30% residual stenosis and there was no blood flow limited dissection after pretreatment) from April 2015 to November 2016 in Guangdong general hospital. The data of basic characteristics,procedures,devices and follow-up information were retrieved and analyzed. The primary endpoint was the composite of cardiac death, recurrent myocardial infarction and target lesion revascularization. (1)The age was (63.3±10.3) years. There were 68.4%(52/76) acute coronary syndrome patients, prevalence of type 2 diabetes was 36.8%(28/76), and 64.5%(49/76)patients with at least one high bleeding risk. (2)The lesion length was (17.4±7.6)mm, and the stenosis was (88.1±8.2)%.The reference vessel diameter≥2.75 mm accounted for 51.2% (41/80), and bifurcation stenosis accounted for 67.5%(54/80). (3)53.7%(43/80) lesions were pretreated with scoring balloon to optimize plaque modification. The paclitaxel-eluting balloon length and diameter were (22.3±5.5)mm and (2.74±0.52)mm.The residual stenosis was (12.3±10.3)%. Procedural success was 88.8%(71/80).Bail-out stenting rate was 5.0%(4/80). (4)The median follow-up duration was 12(6, 25) months. Primary endpoint occurred in 3 cases (3.9%), including 2 cardiac deaths(1 patient died of recurrent myocardial infarction, and 1 patient died of acute heart failure induced by severe mitral insufficiency), and one patient receivedtarget lesion revascularization. In case of no more than 30% residual stenosis and no blood flow limited dissection after lesion pretreatment,it is safe and feasible to treat de novo coronary lesionsusing paclitaxel-eluting balloon.
[Mh] Termos MeSH primário: Síndrome Coronariana Aguda/terapia
Angioplastia Coronária com Balão
Stents Farmacológicos
Paclitaxel/administração & dosagem
Moduladores de Tubulina/administração & dosagem
[Mh] Termos MeSH secundário: Idoso
Angiografia Coronária
Diabetes Mellitus Tipo 2
Feminino
Seres Humanos
Masculino
Meia-Idade
Estudos Prospectivos
Estudos Retrospectivos
Stents
Fatores de Tempo
Resultado do Tratamento
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Tubulin Modulators); P88XT4IS4D (Paclitaxel)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180214
[Lr] Data última revisão:
180214
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180129
[St] Status:MEDLINE
[do] DOI:10.3760/cma.j.issn.0253-3758.2018.01.007


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[PMID]:29247640
[Au] Autor:Gilmore SP; Gonye ALK; Li EC; Espinosa de Los Reyes S; Gupton JT; Quintero OA; Fischer-Stenger K
[Ad] Endereço:Department of Biology, University of Richmond, VA 23173, USA. Electronic address: samuel.gilmore@richmond.edu.
[Ti] Título:Effects of a novel microtubule-depolymerizer on pro-inflammatory signaling in RAW264.7 macrophages.
[So] Source:Chem Biol Interact;280:109-116, 2018 Jan 25.
[Is] ISSN:1872-7786
[Cp] País de publicação:Ireland
[La] Idioma:eng
[Ab] Resumo:The Nuclear Factor-kappa B (NF-κB) pathway is vital for immune system regulation and pro-inflammatory signaling. Many inflammatory disorders and diseases, including cancer, are linked to dysregulation of NF-κB signaling. When macrophages recognize the presence of a pathogen, the signaling pathway is activated, resulting in the nuclear translocation of the transcription factor, NF-κB, to turn on pro-inflammatory genes. Here, we demonstrate the effects of a novel microtubule depolymerizer, NT-07-16, a polysubstituted pyrrole compound, on this process. Treatment with NT-07-16 decreased the production of pro-inflammatory cytokines in RAW264.7 mouse macrophages. It appears that the reduction in pro-inflammatory mediators produced by the macrophages after exposure to NT-07-16 may be due to activities upstream of the translocation of NF-κB into the nucleus. NF-κB translocation occurs after its inhibitory protein, IκB-α is phosphorylated which signals for its degradation releasing NF-κB so it is free to move into the nucleus. Previous studies from other laboratories indicate that these processes are associated with the microtubule network. Our results show that exposure to the microtubule-depolymerizer, NT-07-16 reduces the phosphorylation of IκB-α and also decreases the association of NF-κB with tubulin which may affect the ability of NF-κB to translocate into the nucleus. Therefore, the anti-inflammatory activity of NT-07-16 may be explained, at least in part, by alterations in these steps in the NF-κB signaling pathway leading to less NF-κB entering the nucleus and reducing the production of pro-inflammatory mediators by the activated macrophages.
[Mh] Termos MeSH primário: Transdução de Sinais/efeitos dos fármacos
Moduladores de Tubulina/farmacologia
[Mh] Termos MeSH secundário: Animais
Sobrevivência Celular/efeitos dos fármacos
Citocinas/análise
Citocinas/genética
Citocinas/metabolismo
Regulação para Baixo/efeitos dos fármacos
Ensaio de Imunoadsorção Enzimática
Mediadores da Inflamação/metabolismo
Lipopolissacarídeos/toxicidade
Macrófagos/citologia
Macrófagos/efeitos dos fármacos
Macrófagos/metabolismo
Camundongos
Microscopia de Fluorescência
Inibidor de NF-kappaB alfa/metabolismo
NF-kappa B/metabolismo
Fosforilação/efeitos dos fármacos
Pirróis/química
Pirróis/farmacologia
Células RAW 264.7
Reação em Cadeia da Polimerase em Tempo Real
Moduladores de Tubulina/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Cytokines); 0 (Inflammation Mediators); 0 (Lipopolysaccharides); 0 (NF-kappa B); 0 (Pyrroles); 0 (Tubulin Modulators); 139874-52-5 (NF-KappaB Inhibitor alpha)
[Em] Mês de entrada:1801
[Cu] Atualização por classe:180210
[Lr] Data última revisão:
180210
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171217
[St] Status:MEDLINE



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